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Terazosin HCl Dihydrate Adrenergic Receptor antagonist

Cat.No.S2059

Terazosin HCl is a selective α1-adrenoceptor antagonist, used for treatment of symptoms of an enlarged prostate (BPH).
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Quality Control

Batch: S205901 DMSO]26 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.97%
99.97

Solubility

In vitro
Batch:

DMSO : 26 mg/mL (56.53 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 459.92 Formula

C19H25N5O4.HCl.2H2O

Storage (From the date of receipt)
CAS No. 70024-40-7 Download SDF Storage of Stock Solutions

Synonyms N/A SMILES COC1=C(C=C2C(=C1)C(=NC(=N2)N3CCN(CC3)C(=O)C4CCCO4)N)OC.O.O.Cl

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Mechanism of Action

Targets/IC50/Ki
α-adrenergic receptor
In vitro
Terazosin results in a significant loss of cell viability, via induction of apoptosis in a dose-dependent manner in prostate cancer cells. Terazosin suppresses prostate growth potentially via α 1-adrenoceptor-independent actions gains further support from another study documenting that Doxazosin inhibits proliferation of human vascular smooth muscle cells independently of an antagonistic effect on α1-adrenoceptor. Terazosin blocks HERG currents in Xenopus oocytes with IC50 of 113.2 mM, while Terazosin blocks HERG channel inhibition in human HEK 293 cells with IC50 of 17.7 mM. Terazosin or genistein treatment inhibits the growth of DU-145 cells in a dose-dependent manner, whereas has no effect on normal prostate epithelial cells. Terazosin results in the genistein-induced arrest of DU-145 cells in G2/M phase being overridden and an increase in apoptotic cells, as evidenced by procaspase-3 activation and PARP cleavage. Terazosin induces cytotoxicity in PC-3 and human benign prostatic cells with an IC50 of more than 100 mM.
In vivo
Terazosin significantly inhibits vascular endothelial growth factor induced angiogenesis in nude mice with an IC50 of 7.9 mM, showing that it has a more potent anti-angiogenic than cytotoxic effect. Terazosin also effectively inhibits vascular endothelial growth factor induced proliferation and tube formation in cultured human umbilical vein endothelial cells (IC50 9.9 and 6.8 mM, respectively).
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/12544352/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-09-01)

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